PDE6 Inhibitor

Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.

Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC₅₀ values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma.

TMX-4113 is a FPFT-2216 (HY-145319) (Molecular glue) analog and degrader of PDE6D and CK1α. TMX-4113 does not inhibit the growth of KRAS^G12C-dependent cancer cells. TMX-4113 can be used in the research of multiple myeloma, pancreatic ductal adenocarcinoma, non-small cell lung cancer and gastric adenocarcinoma.

Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC₅₀=0.23 nM). T-0156 inhibits PDE6 (IC₅₀=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC₅₀>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.

Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM respectively, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes^-.

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction.

TPN729 is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729 affects erectile function and it can be used for the research of erectile dysfunction.

PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC₅₀ of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC₅₀s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (K_D=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC₅₀=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD⁺), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.

Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a K_D of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines.

PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC₅₀ of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active.

PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor, with IC₅₀ values of 0.002, 0.180, 2.85 and 2.22 μM against hPDE5, bPDE6, bPDE1 and hPDE3, respectively. PDE5-IN-15 has good oral bioavailability in dogs. PDE5-IN-15 can be used in research on male erectile dysfunction.

PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC₅₀ values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.

PDE4/5-IN-1 is a selective phosphodiesterase 4/5 (PDE4/5) dual inhibitor. PDE4/5-IN-1 functionally inhibits PDE5, PDE4B2, and PDE4D2 activity. PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation in isolated rat prostate tissue, and reduces alpha-1 adrenoceptor-mediated contractile responses in isolated rat prostate tissue. PDE4/5-IN-1 inhibits proliferation of human hyperplastic prostate cells. PDE4/5-IN-1 can be used for the research of benign prostatic hyperplasia.

UK 357903 is a selective inhibitor for phosphodiesterase 5 (PDE5), with IC₅₀s of 1.7 and 714 nM, for PDE5 and PDE6. UK 357903 exhibits vasodilatory effects on the mesenteric and hindlimb vascular beds, and is potential for ameliorating erectile dysfunction.